Tiplaxtinin (PAI-039) is a selective, orally active plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 2.7 uM and Kd of 0.48 uM. Tiplaxtinin (PAI-039) exhibited in vivo oral efficacy in models of acute arterial thrombosis. Tiplaxtinin (PAI-039) inhibited PAI-1 and accelerated fibrinolysis while maintaining normal coagulation in a model of coronary occlusion. Tiplaxtinin (PAI-039) significantly attenuated Ang II-induced aortic medial and wall thickening, enhanced Ang II/salt-induced cardiac fibrosis. Tiplaxtinin (PAI-039) effectively protected from L-NAME-induced thrombosis in murine model of hepatic vein thrombosis.
